JP2017002048A - ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態 - Google Patents

ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態 Download PDF

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Publication number
JP2017002048A
JP2017002048A JP2016123403A JP2016123403A JP2017002048A JP 2017002048 A JP2017002048 A JP 2017002048A JP 2016123403 A JP2016123403 A JP 2016123403A JP 2016123403 A JP2016123403 A JP 2016123403A JP 2017002048 A JP2017002048 A JP 2017002048A
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JP
Japan
Prior art keywords
polymorph
pyrimido
ethyl
mesitylimino
dimethoxy
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2016123403A
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English (en)
Japanese (ja)
Inventor
ウォーカー，マイケル，ジェイ．，エー．
J A Walker Michael
プルヴィエ，ベルトラン，エム．，シー．
M C Plouvier Bertrand
ノーザン，ジュリアン，エス．
S Northen Julian
フェルナンデス，フィリップ
Fernandes Philippe
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Verona Pharma Ltd
Original Assignee
Verona Pharma Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Verona Pharma Ltd filed Critical Verona Pharma Ltd
Publication of JP2017002048A publication Critical patent/JP2017002048A/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016123403A 2010-08-09 2016-06-22 ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態 Pending JP2017002048A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37189210P 2010-08-09 2010-08-09
US61/371,892 2010-08-09

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
JP2013523593A Division JP6038788B6 (ja) 2010-08-09 2011-08-09 ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態

Publications (1)

Publication Number Publication Date
JP2017002048A true JP2017002048A (ja) 2017-01-05

Family

ID=44510951

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016123403A Pending JP2017002048A (ja) 2010-08-09 2016-06-22 ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態

Country Status (21)

Country Link
US (1) US9062047B2 (fr)
EP (1) EP2603509B1 (fr)
JP (1) JP2017002048A (fr)
KR (1) KR101860968B1 (fr)
CN (1) CN103313985B (fr)
AR (1) AR082601A1 (fr)
AU (1) AU2011288497B2 (fr)
BR (1) BR112013003087A2 (fr)
CA (1) CA2807082C (fr)
DK (1) DK2603509T3 (fr)
ES (1) ES2483801T3 (fr)
IL (1) IL224450B (fr)
MX (1) MX345802B (fr)
MY (1) MY157432A (fr)
PH (1) PH12013500261A1 (fr)
PL (1) PL2603509T3 (fr)
PT (1) PT2603509E (fr)
RU (1) RU2577541C2 (fr)
SI (1) SI2603509T1 (fr)
TW (1) TWI516488B (fr)
WO (1) WO2012020016A1 (fr)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2968312B1 (fr) 2013-03-15 2018-01-31 Verona Pharma PLC Association de médicaments
PL3231444T3 (pl) 2014-05-12 2020-05-18 Verona Pharma Plc Nowe leczenie
MY196072A (en) 2014-09-15 2023-03-13 Verona Pharma Plc Liquid Inhalation Formulation Comprising RPL554
GB201502260D0 (en) * 2015-02-11 2015-04-01 Verona Pharma Plc Salt of Pyrimido[6,1-A]Isoquinolin-4-one compound
GB201613054D0 (en) 2016-07-28 2016-09-14 Verona Pharma Plc New compound and process
PT3822272T (pt) 2018-07-13 2025-01-22 Chia Tai Tianqing Pharmaceutical Group Co Ltd Composto tricíclico fundido como inibidor duplo de pde3/pde4
GB2578093B (en) * 2018-10-09 2020-11-18 Verona Pharma Plc Liquid pharmaceutical composition comprising RPL554 and HFA-134A
JP7712276B2 (ja) * 2020-01-15 2025-07-23 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド 三環式ｐｄｅ３／ｐｄｅ４二重阻害剤化合物の医薬組成物
WO2023076205A1 (fr) 2021-10-29 2023-05-04 Teva Pharmaceuticals International Gmbh Formes à l'état solide de l'ensifentrine et leur procédé de préparation
GB202202297D0 (en) 2022-02-21 2022-04-06 Verona Pharma Plc Formulation production process
EP4378942A1 (fr) 2022-12-02 2024-06-05 Sandoz AG Forme cristalline d'un inhibiteur pde3/4
US20260015354A1 (en) * 2022-12-14 2026-01-15 Cipla Limited Solid State Forms of Ensifentrine
AU2024309346C1 (en) 2023-06-26 2026-03-12 Verona Pharma Plc Particulate composition comprising ensifentrine
US20250249008A1 (en) * 2024-02-07 2025-08-07 Verona Pharma Plc Pharmaceutical compositions of ensifentrine for chronic obstructive pulmonary disease
WO2025176871A1 (fr) 2024-02-23 2025-08-28 Inke, S.A. Procédé de préparation de pyrimido[6,1-a]isoquinoléine-4-ones
CN121226374A (zh) * 2025-12-03 2025-12-30 长风药业股份有限公司 一种恩塞芬汀盐型化合物及其成盐方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002540207A (ja) * 1999-03-31 2002-11-26 バーナリス・リミテッド ピリミド［６，１−ａ］イソキノリン−４−オン誘導体
JP6038788B2 (ja) * 2010-08-09 2016-12-07 ヴェローナ ファーマ ピーエルシーＶｅｒｏｎａ Ｐｈａｒｍａ Ｐｌｃ ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2081117C1 (ru) * 1992-09-09 1997-06-10 Глэксо Груп Лимитед Производные лактама или их физиологические приемлемые соли или сольваты
AU2008276451A1 (en) * 2007-07-17 2009-01-22 Zalicus Inc. Treatments of B-cell proliferative disorders

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002540207A (ja) * 1999-03-31 2002-11-26 バーナリス・リミテッド ピリミド［６，１−ａ］イソキノリン−４−オン誘導体
JP6038788B2 (ja) * 2010-08-09 2016-12-07 ヴェローナ ファーマ ピーエルシーＶｅｒｏｎａ Ｐｈａｒｍａ Ｐｌｃ ピリミド［６，１−ａ］イソキノリン−４−オン化合物の結晶形態

Also Published As

Publication number Publication date
MX345802B (es) 2017-02-16
AU2011288497B2 (en) 2016-01-21
DK2603509T3 (da) 2014-09-08
TW201213325A (en) 2012-04-01
RU2013110225A (ru) 2014-09-20
EP2603509B1 (fr) 2014-06-18
KR101860968B1 (ko) 2018-05-24
PT2603509E (pt) 2014-08-29
CA2807082A1 (fr) 2012-02-16
PL2603509T3 (pl) 2014-11-28
SI2603509T1 (sl) 2014-10-30
US9062047B2 (en) 2015-06-23
IL224450B (en) 2018-01-31
US20130225616A1 (en) 2013-08-29
PH12013500261A1 (en) 2013-03-04
ES2483801T3 (es) 2014-08-07
KR20140009112A (ko) 2014-01-22
MX2013001533A (es) 2013-06-07
MY157432A (en) 2016-06-15
CA2807082C (fr) 2017-07-25
TWI516488B (zh) 2016-01-11
CN103313985A (zh) 2013-09-18
JP6038788B2 (ja) 2016-12-07
WO2012020016A1 (fr) 2012-02-16
AR082601A1 (es) 2012-12-19
RU2577541C2 (ru) 2016-03-20
CN103313985B (zh) 2016-03-02
BR112013003087A2 (pt) 2016-07-05
JP2013533301A (ja) 2013-08-22
EP2603509A1 (fr) 2013-06-19
AU2011288497A1 (en) 2013-03-14

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